Flunitrazepam

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient flunitrazepam belongs to the so-called benzodiazepines and is used as a sleeping and sedative. Its use should be as short as possible, otherwise a dependency will develop quickly. Here you can find out everything you need to know about flunitrazepam: effect, use and side effects.

This is how flunitrazepam works

The signal transmission between the nerve cells in the brain takes place via narrow, gap-like contact points (so-called synapses): One cell releases a messenger substance (neurotransmitter) into the synaptic gap, which binds to suitable docking points (receptors) of the subsequent cell and in this way removes it is perceived. Depending on the type of neurotransmitter and receptor, the signal can be either excitatory or inhibitory. The messenger substance GABA (gamma-aminobutyric acid), for example, transmits an inhibitory signal to the GABA receptor. If this signal path is stimulated by drugs such as flunitrazepam, the patient first becomes calmer, then tired and finally falls asleep.

In contrast to barbiturates, which were previously often used as sleep aids, benzodiazepines do not imitate the neurotransmitter GABA. Instead, they change the GABA receptor so that it reacts more strongly to the body's own GABA. Thus, the body has a way to regulate the effect.This is particularly important for long-term use, since with flunitrazepam and other active ingredients in the group, tolerances occur after just a few weeks - despite the same dosage, the effectiveness decreases, which creates the need for higher dosages.

Flunitrazepam uptake, breakdown and excretion

After ingestion as a tablet on an empty stomach, the active ingredient is quickly and almost completely absorbed into the blood through the intestinal wall. After about twenty minutes, half of the ingested active ingredient has already reached the bloodstream and crosses the blood-brain barrier into the brain. The active ingredient is broken down in the liver and excreted in the urine via the kidneys. About one day after ingestion, half of the active ingredient has already left the body.

When is flunitrazepam used?

The active ingredient flunitrazepam is approved as a tablet for the short-term treatment of sleep disorders, but is now almost irrelevant in this area of ​​application.

In addition, it is approved as an injection solution for calming before and after surgical and diagnostic interventions and is used particularly in intensive care medicine.

The treatment must be as short as possible, otherwise it can quickly lead to habituation and dependency. If flunitrazepam is used for more than a week, spontaneous discontinuation often leads to withdrawal symptoms.

This is how flunitrazepam is used

To treat sleep disorders, flunitrazepam is taken as a tablet just before going to bed. The usual dosage is half a milligram to one milligram flunitrazepam at night. Older patients in particular should not get up after taking it, as there is an increased risk of falling. If the active ingredient has been used for more than a week, it should be gradually withdrawn ("tapered") to end the treatment.

Treatment with flunitrazepam as a solution for injection is reserved for doctors.

What are the side effects of flunitrazepam?

The adverse drug reactions (ADRs) while taking flunitrazepam are mostly due to its central depressant effect. Possible side effects include double vision, nausea, vomiting, skin reactions with redness, itching and swelling, muscle weakness, falls and broken bones, heart failure and cardiac arrest. In addition, breathing can slow down or even stop breathing. This risk is particularly acute in the case of lung dysfunction (such as asthma and COPD), brain damage or the simultaneous use of other drugs with the same side effects.

What should be considered when taking flunitrazepam?

Since the sleeping pill flunitrazepam is broken down in the liver via enzymes that also break down other drugs, taking it at the same time can lead to interactions. The effect of flunitrazepam and the other active ingredients can be both weakened and increased. Medicines against fungal infections (ketoconazole, fluconazole), HIV drugs, antibiotics (erythromycin, clarithromycin), cholesterol-lowering drugs (atorvastatin, simvastatin) and high blood pressure drugs (verapamil) lead to an increased effect of flunitrazepam. Grapefruit juice can also increase the effects of flunitrazepam.

Conversely, epilepsy drugs such as phenobarbital, phenytoin and carbamazepine can accelerate the breakdown of flunitrazepam and thus reduce its effect.

With simultaneous use of active ingredients that have a calming or sleep-promoting effect as a side effect, the effect of flunitrazepam can increase in an unpredictable way. These include other sleeping pills and tranquilizers, anti-anxiety medication, anti-allergy drugs, antidepressants, neuroleptics, and anti-seizure drugs.

Patients should not operate heavy machinery or drive vehicles while being treated with flunitrazepam.

Older patients in particular can react paradoxically to treatment with flunitrazepam: Instead of a calming and sleep-inducing effect, aggressive behavior, delusions and excitability can develop.

The active ingredient flunitrazepam should not be taken during pregnancy (especially in the last trimester) and breastfeeding, as it can cause massive symptoms of intoxication in the child.

Children, patients with severe liver dysfunction and people with (previous) addiction disorders must not be treated with flunitrazepam.

How to get flunitrazepam medication

In contrast to other benzodiazepines, flunitrazepam is not listed as an “exempt preparation” in the German Narcotics Act (BtmG). That means: All other benzodiazepines may be sold in pharmacies as prescription drugs below a certain dosage and pack size. Flunitrazepam, on the other hand, may only be dispensed in any dosage and pack size in accordance with a prescription on a yellow narcotic prescription in the pharmacy.

How long has flunitrazepam been known?

The sleeping pill Flunitrazepam was developed by the pharmaceutical company Hoffmann-La Roche and patented in 1972. It was first launched in 1975 in several European countries. Because of the potential for abuse, a single dose (tablet) has not been allowed to contain more than one milligram of active ingredient since 1998 (previously there were also tablets with two milligrams of flunitrazepam each). After the patent protection expired, several generics with the active ingredient flunitrazepam came onto the market.

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